2009 Fiscal Year Final Research Report
Research of retinoic acid-modified nuclear receptor agonist
| Project/Area Number |
20790105
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | Kobe Pharmaceutical University |
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Principal Investigator |
OKITSU Takashi Kobe Pharmaceutical University, 薬学部, 助教 (50441209)
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| Project Period (FY) |
2008 – 2009
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| Keywords | 医薬分子設計 / 核内受容体 / レチノイド / RXR / RAR |
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| Research Abstract |
The ligand molecules of retinoid X receptors (RXRs) are candidates for therapeutic agents of metabolic syndrome such as dyslipidemia and type II diabete. The natural ligand of RXR is 9Z-retinoic acid so that I have developed an efficient synthesis of 9Z-rerinoic acid and its analogs. Among them, (-)-menthol congener had strong RXRα agonist activity. It is noteworthy that an analog having indole showed isotype selectivity (RXRα>γ). In the process of my project, I also discovered novel iodocyclizations leading to benzofurans and spiro compounds.
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[Journal Article] Mild and efficient deprotection of acetal-type protecting groups of hydroxyl functions by triethylsilyl triflate-2, 4, 6-collidine combination2009
Author(s)
Fujioka, H.; Kubo, O.; Okamoto, K.; Senami, K.; Okitsu, T.; Ohnaka, T.; Sawama, Y.; Kita, Y.
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Journal Title
Heterocycles 77
Pages: 1089-1103
Peer Reviewed
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